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N-Desmethylclozapine exerts dual and opposite effects on salivary secretion in the rat.

Artikel i vetenskaplig tidskrift
Författare Jörgen Ekström
Tania Godoy
Alessandro Riva
Publicerad i European journal of oral sciences
Volym 118
Nummer/häfte 1
Sidor 1-8
ISSN 1600-0722
Publiceringsår 2010
Publicerad vid Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi
Sidor 1-8
Språk en
Länkar dx.doi.org/10.1111/j.1600-0722.2009...
Ämnesord Adrenergic alpha-Antagonists, pharmacology, Adrenergic beta-Agonists, pharmacology, Animals, Blood Pressure, drug effects, Clozapine, analogs & derivatives, pharmacology, Denervation, Drug Synergism, Female, Isoproterenol, pharmacology, Muscarinic Agonists, pharmacology, Parotid Gland, drug effects, Rats, Rats, Sprague-Dawley, Receptor, Muscarinic M1, agonists, Saliva, secretion, Salivation, drug effects, Secretory Rate, Submandibular Gland, drug effects
Ämneskategorier Fysiologi, Farmakologisk forskning

Sammanfattning

N-Desmethylclozapine is a major metabolite of the atypical antipsychotic drug clozapine, used in the treatment of therapy-resistant schizophrenia. Patients under clozapine treatment report a troublesome sialorrhea. Recent experiments show clozapine to exert mixed agonist/antagonist actions on salivary secretion in rats. The present study was performed to define the secretory role of N-desmethylclozapine and to compare it with that of its parent compound. N-Desmethylclozapine evoked secretion by acting directly on the muscarinic acetylcholine M1-receptors of 'silent' duct-cannulated parotid and submandibular glands of the anaesthetized rat. In chronic surgically denervated glands, the secretory response was enlarged. The methacholine-evoked secretion, as well as the parasympathetic nerve-evoked secretion, were reduced by N-desmethylclozapine and involved blockade of M3-receptors, while the sympathetic nerve-evoked response was reduced, involving blockade of alpha(1)-adrenergic receptors. Synergistic interactions between N-desmethylclozapine and the beta-adrenergic receptor agonist, isoprenaline, occurred. Compared with clozapine, the excitatory efficacy of N-desmethylclozapine was higher and the inhibitory efficacy was lower (parasympathetic activity) or about the same (sympathetic activity). Theoretically, in humans treated with clozapine, an increase in the N-desmethylclozapine : clozapine ratio would contribute to salivation during the night and at rest, and, furthermore, the magnitude of the reduction in the reflexly elicited secretion is likely to diminish.

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